Z3. Pharmacology p307
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- glaucoma drugs
- p. 307
- which alpha agonists are used to treat glaucoma
- epinephrine, brimonidine
- which beta blockers are used to treat glaucoma
- timolol, betxolol, carteolol
- which cholinomimetics are used to treat glaucoma
- pilocarpine, carbachol, physostigmine, echothiophate
- which diuretics are used to treat glaucoma
- acetazolamide, dorzolamide, brinzolamide
- which prostaglandin is used to treat glaucoma
- latanoprost
- what classes of drugs are used to treat glaucoma
- alpha agonists, beta blockers, cholinomimetics, diuretics, prostaglandins (*mnemonic -- treating glaucoma is easy as ABCD)
- what is the effect of epinephrine in glaucoma
- increase outflow of aqueous humor
- what are the side effects of epinephrine treatment in glaucoma
- mydriasis, stinging
- what glaucoma should epinephrine NOT be used for
- closed-angle glaucoma
- what is the effect of brimonidine in glaucoma
- decreased aqueous humor synthesis
- what are the side effects of brimonidine treatment in glaucoma
- no pupillary or vision changes
- what is the effect of beta-blocker treatment in glaucoma
- decrease aqueous humor secretion
- what are the side effects of beta blocker treatment in glauzoma
- no pupillary or vision changes
- what is the effect of cholinomimetics in glaucoma
- ciliary muscle contraction, opening of trabecular meshwork, increase outflow of aqueous humor
- what are the side effects of cholinomimetics in glaucoma
- miosis, cyclospasm
- what is the effect of diuretic treatment in glaucoma
- inhibition of carbonic anhydrase --> decrease HCO3 secretion --> decrease aqueous humor secretion
- what are the side effects of diuretics in glaucoma
- no pupillary or vision changes
- what is the effect of prostaglandin (latanoprost) treatment in glaucoma
- increase outflow of aqueous humor
- what is the side effect of prostaglandin treatment in glaucoma
- darkens color of iris (browning)
- which drugs used to treat glaucoma increase outflow of aqueous humor
- cholinomimetics, prostaglandin, epinephrine
- can you use epinephrine in closed-angle glaucoma
- NO
- brimonidine is used to treat what eye disease
- glaucoma
- what kind of drug is latanoprost
- prostaglandin
- latanoprost is used to treat what eye disease
- glaucoma
- which glaucoma drugs decrease aqueous secretion
- beta blockers, diuretics
- L-dopa/carbidopa
- p. 307
- what does L-dopa stand for
- levodopa
- what is the mechanism of action of L-dopa/carbidopa
- increase dopamine level in brain
- what is L-dopa/carbidopa used to treat
- Parkinson's disease
- how is L-dopa different from dopamine
- L-dopa can cross the blood-brain barrier, dopamine cannot
- what happens to L-dopa after it crosses the BBB
- converted to dopamine by dopa decarboxylase
- what enzyme convertes L-dopa to dopamine
- dopa decarboxylase
- what is the function of carbidopa
- peripheral decarboxylase inhibitor
- why is carbidopa given with L-dopa
- increase L-dopa availability in CNS by inhibiting decarboxylase in periphery, also limits peripheral side effects
- what are the side effects of L-dopa.carbidopa treatment
- arrhythmias, dyskinesias
- why do patients taking L-dopa get arrhythmias
- peripheral effects of dopamine
- why do patients taking L-dopa get dyskinesias
- excess dopamine stimulation in CNS
- Parkinson's disease drugs
- p.308
- what drugs are used to treat Parkinson's disease
- dopamine agonists, MAO inhibitors, antimuscarinics
- specifically, which drugs are used to treat Parkinson's
- Bromocriptine, Amantadine, Levodopa, Selegiline, Antimuscarinics (BALSA)
- which dopamine agosts are used to treat Parkinson's
- L-dopa/carbidopa, bromocriptine, pramipexole, ropinirole, amantadine
- what is the action of bromocriptine in Parkinson's
- ergot alkaloid, partial dopamine agonist
- what is the action of amantadine in Parkinson's
- enhances dopamine release
- what MAOI is used to treat Parkinson's
- selegiline
- what is the mechanism of selegiline
- selective MAO type B inhibitor
- what antimuscarinic is used to treat Parkinson's
- benztropine
- what is the effect of benztropine in Parkinson's
- improves tremor, rigidity, little effect on bradykinesia
- Sumatriptan
- p. 308
- what is sumatriptan used for
- acute migraine, cluster headache attacks
- what is the mechanism of sumatriptan
- 5-HT1D agonist
- what is the half life of sumatriptan
- less than 2 hours
- what are the side effects of sumatriptan
- chest discomfort, mild tingling
- what are the contraindications for sumatriptan
- patients with CAD or Prinzmetal's angina
- Epilepsy drugs
- p. 308
- which drugs are used for simple and complex partial seizures
- phenytoin, carbamazapine, lamotrigine, gabapentin, topiramate, phenobarbital
- what types of seizures is phenytoin indicated for
- simple and complex partial, tonic-clonic, status epilepticus
- what types of seizures is carbamazepine indicated for
- simple and complex partial, tonic-clonic
- what types of seizures is lamotrigine indicated for
- simple and complex partial, tonic-clonic
- what types of seizures is gabapentin indicated for
- simple and complex partial, tonic-clonic
- what types of seizures is topiramate indicated for
- simple and complex partial
- what types of seizures is phenobarbital indicated for
- simple and complex partial, tonic-clonic
- what drugs can be used for tonic-clonic seizures
- phenytoin, carbamazapine, lamotrigine, gabapentin, phenobarbital, valproate
- what drugs can be used for absence seizures
- valproate, ethosuximide
- what drugs can be used for status epilepticus
- phenytoin, benzodiazapines (diazepam, lorazepam)
- what types of seizure is valproate indicated for
- tonic-clonic, absence
- what types of seizure is ethosuximide inidcated for
- absence
- what type of seizure are benzodiazepines indicated for
- status epilepticus
- other than anti-seizure, what else is phenytoin used for
- class 1B anti-arrhythmic
- how should a patient taking carbamazepine be followed
- monitor LFT's weekly
- which seizure drugs have adjunct use
- gabapentin, topiramate
- which seizure drug is safest in pregnant women
- phenobarbital
- which seizure drug is used in Crigler-Najjar II
- phenobarbital
- what are the advantages of phenobarbital
- can be used in pregnant women, Crigler Najjar II
- Epilepsy drug toxicities
- p. 309
- what are the side effects of benzodiazepines
- sedation, tolerance, dependence
- what are the side effects of carbamazepine
- diplopia, ataxia, CYP induction, blood dyscrasias, liver toxicity
- what are the side effects of ethosuximide
- GI distress, lethargy, headache, urticaria, Stevens-Johnson syndrome
- what are the side effects of phenobarbital
- sedation, CYP induction, tolerance, dependence
- what are the side effects of phenytoin
- nystagmus, diplopia, ataxia, sedation, ginigival hyperplasia, hirsutism, anemias, teratogenic
- what are the side effects of valproate
- GI distress, rare by fatal hepatotoxicity, neural tube defects (spina bifida)
- what are the side effects of lamotrigine
- life-threatening rash, Stevens-Johnson syndrome
- what are the side effects of gabapentin
- sedation, movement disorders
- what are the side effects of topiramate
- sedation, mental dulling, kidney stones, weight loss
- which anti-epileptic drug is teratogenic
- phenytoin
- which anti-epileptic drug can cause dependence
- benzodiazepines, phenobarbital
- which anti-epileptic drug can cause neural tube defects
- valproate
- which anti-epileptic drugs can cause GI distress
- valproate, ethosuximide
- it is necessary to check LFT's with which anti-epileptic drugs
- carbamazepine, valproate
- which anti-epileptic drugs cause CYP induction
- phenobarbital, carbamazepine
- which anti-epileptic drugs can cause blood problems
- carbamazepine, phenytoin
- which anti-epileptic drugs can cause Stevens-Johnson syndrome
- lamotrigine, ethosuximide
- which anti-epileptic drugs can cause diplopia
- carbamazepine, phenytoin
- Phenytoin
- p. 309
- what is the mechanism of phenytoin action
- use-dependent blockade of Na+ channels
- what is the clinical application of phenytoin
- grand mal seizures
- what are the toxicities of phenytoin
- nystagmus, ataxia, diplopia, lethargy
- what are the chronic toxicities of phenytoin
- gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia, malignant hyperthermia (rare)
- should pregnant women take phenytoin
- NO -- teratogenic
- why does phenytoin cause megaloblastic anemia
- causes decreased vitamin B-12
- Barbiturates
- p. 309
- name 4 barbiturates
- phenobarbital, pentobarbital, thiopental, secobarbital
- what is the mechanism of barbiturate action
- increase duration of Cl channel opening --> decreased neuron firing --> facilitate GABA-A action
- how do barbiturates facilitate GABA-A action
- increase duration of Cl channel opening which decreases neuron firing (Barbidurate increases duration
- is barbiturate action on the CNS stimulatory or inhibitory
- inhibitory
- what is the clinical application of barbiturates
- sedative for anxiety, seizures, insomnia, anesthesia induction (thiopental)
- which barbiturate is used for anesthesia induction
- thiopental
- what are the side effects of barbiturates
- dependence, additive CNS depression effects with alcohol, respiratory or CV depression (death), drug interactions due to CYP induction
- what should you find out before giving a patient barbiturates
- what other medications they take, because of CYP induction and many drug interactions
- what happens if you give barbiturates to a patient in alcohol-induced coma or DT's
- they might DIE!! Because of additive effect of barbiturates and alcohol --> respiratory depression
- when are barbiturates contra-indicated
- porphyria
- can barbiturates cause dependence
- YES
- My friend Barb was very anxious so her doctor gave her barbiturates to increase the duration of the time she could speak in public without freaking out and having a seizure. She became so dependent on it that she recommended it to her friend Portia who
- clinical pharmacology made ridiculous. Period
- Benzodiazepines
- p. 309
- name a bunch of benzodiazepines
- diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide (all have ZZZ in them)
- what is the mechanism of benzodiazepines
- increase frequency of Cl channel opening --> facilitate GABA-A action (Frenzodiazepines increase frequency)
- which GABA receptors are facilitated by barbiturates and bezodiazepines
- GABA-A
- what are the clinical applications of benzodiazepines
- anxiety, spasticity, status epilepticus (diazepam), detoxification (alcohol withdrawal, DT's)
- which benzodiazepine can be used for status epilepticus
- diazepam
- what drugs can be used to treat alcohol withdrawal
- benzodiazepines
- which benzodiazepines are short-acting
- TOM thumb: Triazolam, Oxazepam, Midazolam
- what are the toxic effects of benzos
- dependence, additive CNS depression effects with alcohol
- how are benzos better than barbiturates
- less respiratory depression and coma risk
- how do you treat benzo overdose
- flumazenil
- what is flumzenil used for
- benzo overdose
- how does flumazenil work
- competitive antagonist at GABA receptor
- can a patient become benzodiazepine dependent
- YES
- are barbiturates or benzodiazepines used for alcohol withdrawal
- benzodiazepines
- Antipsychotics (neuroleptics)
- p. 310
- what is another name for antipsychotics
- neuroleptics
- name 4 antipsychotic drugs
- thioridazine, haloperidol, fluphenazine, chlorpromazine
- how do you keep benzos straight from antipsychotics
- Benzos help 3rd year Jon Kazam be less anxious around patients: Shazam Kazam! Without antipsychotics patients talk like a crazy 'zine (well, not perfect, but I'm working on it)
- what is the mechanism of most antipsychotics
- block dopamine D2 receptors
- what is the clinical application of antipsychotics
- schizophrenia, psychosis
- what are the side effects of antipsychotics
- extrapyramidal side effects (EPS), sedation, endocrine, muscarinic blockade, alpha blockade, histamine blockade
- what is a long-term effect of antipsychotic use
- tardive dyskinesia
- what is neuroleptic malignant syndrome
- a side effect of antipsychotics; rigidity, autonomic instability, hyperpyrexia
- how do you treat neuroleptic malignant syndrome
- dantrolene, dopamine agonists
- what is tardive dyskinesia
- side effect of neuroleptics; stereotypic oral-facial movements, may be due to dopamine receptor sensitization
- what is the "rule of 4" with EPS side effects from antipsychotic drugs
- evolution of EPS side effects: 4 hours -- acite dystonia, 4 days -- akinesia, 4 weeks -- akasthesia, 4 months -- tardvie dyskinesia
- is tardvie dyskinesia reversible
- often irreversible
- what is fluphenazine used for
- schizophrenia, psychosis
- Atypical antipsychotics
- p. 310
- name 3 atypical antipsychotics
- clozapine, olanzapine, risperidone
- what type of antipsychotic is clozapine
- atypical
- what type of antipsychotic is olanzapine
- atypical
- what type of antipsychotic is risperidone
- atypical
- what is the mechanism of atypical antipsychotics
- block 5-HT2 and dopamine receptors
- what is the mechanism of clozapine
- block 5-HT2 and dopamine receptors
- what is the mechanism of olanzapine
- block 5-HT2 and dopamine receptors
- what is the mechanism of risperidone
- block 5-HT2 and dopamine receptors
- what is the clinical application of clozapine
- schizophrenia positive and negative symptoms
- what is the clinical application of olanzapine
- schizophrenia positive and negative symptoms, OCD, anxiety disorder, depression
- what is the clinical application of risperidone
- schizophrenia positive and negative symptoms
- how are atypical antipsychotics different from classic ones
- atypicals treat positive and negative symptoms of schizophrenia, fewer extrapyramidal and anticholinergic side effects than classic antipsychotics
- which antipsychotics should be used to treat positive and negative symptoms of schizophrenia
- atypical ones -- clozapine, olanzapine, risperidone
- which antipsychotics should be used for fewer side effects
- atypical ones -- clozapine, olanzapine, risperidone
- what is a potential toxicity of clozapine
- agranulocytosis
- which antipsychotic drug can cause agranulocytosis
- clozapine
- what test must be done weekly on patients taking clozapine
- WBC count because of potential agranulocytosis
- Lithium
- p. 310
- what is the mechanism of action of lithium
- unknown; may be related to inhibition of phosphoinositol cascade
- what is the clinical application of lithium
- mood stabilizer for bipolar disorder
- how does lithium help people with bipolar disorder
- prevents relapse and acute manic episodes
- what are the side effects of lithium
- tremor, hypothyroidism, polyuria, teratogenic
- is it OK for women taking lithium to get pregnant
- NO -- teratogenic
- what does lithium cause polyuria
- ADH antagonist --> nephrogenic diabetes insipidus
- Antidepressants
- pg 311
- What do the following drugs inhibit: 1. MAO inhibitors, 2. Desipramine/maprotilline, 3. Mirtazapine and 4. Fluoxetine/trazodone?
- 1. MAO 2. NE reuptake 3. Alpha 2-R 4. 5HT reuptake
- All of the above actions are ------synaptic
- PRE
- List the Tricyclic Antidepressants
- pg 311 Imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin
- What are the three C's of their toxicity?
- Convulsions, Coma, Cardiotoxicity (arrythmias). Also respiratory depression, hypyrexia.
- How about toxicity in the eldery?
- confusion and hallucinations due to anticholinergic SE
- What is the mechanism of TCA?
- block reuptake of NE and 5HT
- What is the clinical uses of TCAs?
- Endogenous depresion. Bed wetting - imipramine. OCD- clomipramine.
- How are tertiary TCA's different than secondary in terms of side effects?
- Amitriptyline (tertiary) has more anti-cholinergic effects than do secondary (nortriptyline). Desipramine is the least sedating.
- what are the SE of TCAs?
- sedation, alpha blocking effects, atropine-like anti cholinergic side effects (tachycardia, urinary retention)
- Fluoxetine, sertraline, paroxetine, citalopram are what class of drugs?
- pg 311 SSRI's for endogenous depression
- How long does it take an anti-depressant to have an effect?
- 2-3weeks
- How does the toxicity differ fromTCA's and what are they?
- Fewer than TCA's. CNS stimulation - anxiety, insomnia, tremor, anorexia, nausea, and vomiting.
- What toxicity happens with SSRI's and MAO inhibitors given together?
- Seratonin Syndrome! Hyperthermia, muscle rigidity, cardiovascular collapse
- What are heterocyclics?
- pg 312 2nd and 3rd generation antidepressants with varied and mixed mechanisms of action. Used major depression.
- Examples of heterocyclics?
- trazodone, buproprion, venlafaxine, mirtazapine, maprotiline
- Which one is used for smoking cessation?
- Buproprion. Mechanism not known. Toxicity - stimulant effects, dry mouth, aggrevation of pyschosis
- Which one used in GAD?
- Venlafaxine - inhibits 5HT and DA reuptake. Toxicity - stimulant effects
- which one blocks NE reuptake
- maprotiline
- Which one increases release of NE and 5HT via alpha 2 antagonism?
- mirtazapine. Also potent 5HT Rantagonist. Toxicity - sedation, increase serum cholesterol, increase appetite
- What is trazodone and it' SE?
- primarily inhibits seratonin reuptake. Toxicity - sedation, nausea, priapism, postural hypotension
- Give 2 examples of MAO
- pg 312 phenelzine. Tranylcypromine
- Mechanism and Clinical Uses?
- non selevtive MAO inhibition. Atypical antidepressant, anxiety, hypochondriasis
- What is the toxicity with tyramine ingestion (in foods) and meperidine?
- Hypertensive crisis
- Other toxicities?
- CNS stimulation, contraindicated with SSRI's or B-agonists
- What is the mechanims of selgiline (deprenyl)?
- pg 312 Selectively inhibits MAO-B, increasing DA
- what is the clinical use and toxicity?
- adjunctive agent to L-dopa for Parkinsons. May enhance adverse effects of L-dopa
- Analgesics/ Anesthetics
- pg 312
- General principles
- pg 312
- What is the significance of drugs with decreased solubility in blood?
- rapid induction and recovery times . Ie. N20
- What is the significance of drugs with increased solubility in blood?
- increased potency = I/ MAC. Ie. Halothane
- Inhaled Anesthetics
- pg 312
- list them
- halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
- What is good about lower solubility?
- the quicker the anesthetic response, and the quicker the recovery
- What are these drug's effects?
- myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow
- What toxicity mactches the following drugs 1. Halothane 2. Methoxyflurane 3. Enflurane 4. Rare
- 1. Hepatotoxcity 2. Nephrotoxicty 3. Proconvulsant 4. Malignant hyperthermia
- IV anesthetics
- pg313
- What do barbituates, benzodiazepines, arylcyclohexylamines and narcotic analgesics have in common?
- they are IV anesthetics
- What the pharmacokinetics and uses of thiopental?
- high lipid solubility, rapid entry into brain. Used for induction of anesthesia for short surgical procedures. Terminated by redistribution from brain. Decreased cerebral blood flow
- Give an example of a benzo and what is this class's shortcoming?
- midazolam used for endoscopy. Used with gaseous anesthetics and narcotics. May cause severe post-op respiratory depressio and amnesia
- What does Ketamine (PCP analog and an arylcyclohexylamine) do?
- dissociative anesthetic. Cardiovascular stimulant. Causes disorientation, hallucination, bad dreams. Increases cerebral blood flow.
- How are narcotic analgesics used? Examples?
- Morphone and fentanyl are used with CNS depressant during general anesthesia.
- What is the advantage of propofol
- used for rapid anesthesia induction and short procedures. Less post-op nausea than thiopental
- Local anesthetics
- pg 313
- Name some esters?
- procaine, cocaine, tetracaine,
- Name some amides?
- lidocaine, bupivacaine, (amides have two I's in name!)
- What is the mechanism and clinical use?
- bind receptor and block Na channels. Tertiary amine local anesthetics penetrate membrane in uncharge form, then bind charged form. Use for minor surgical procedures, spinal anesthesia.
- How do you decide to use ester or amides?
- if allergic to esters, give amides
- what is the toxicity
- CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, arrhythmias (cocaine)
- In infected ________ tissue, anesthetics are charged and cannot penetrate membrane. Therefore, ______ anesthetics are needed.
- acidic; more
- What is the order of nerve blockade for size and myelination? Which factor predominates?
- small diameter> large diameter. Myelinated fibers> unmyelinated fibers. Size factor predominates
- what is the order of loss of sensation?
- pain first, then temp, then touch, then pressure
- Why would you give these drugs with vasoconstrictors?
- to enhance local action
- Opiod analgesics
- pg 313
- List as many as you can.
- morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
- Mechanism: They act as _____ for opiod receptors to modulate synaptic transmission
- agonists
- which drugs act at the mu, delta, kappa receptors?
- morphine enkephalin, dynorphin
- Clinical use?
- pain, cough supression (dex), diarrhea (loperamide), acute pulmonary edema, methadone maintenance programs
- What are the major toxicities?
- addiction, respiratory depression, constipation, miosis, additive CNS depression wth other drugs
- Tolerance does not develop to __________and ______
- miosis and constipation
- How would you treat toxicity?
- naloxone, naltrexone (opiod R antagonist)